Jiang Liang, Wang Xiaolu, Wang Yuting, Xu Fang, Zhang Zhang, Ding Ke, Lu Xiaoyun
International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE) , School of Pharmacy , Jinan University , 601 Huangpu Avenue West , Guangzhou 510632 , China . Email:
RSC Med Chem. 2020 Feb 12;11(2):293-296. doi: 10.1039/c9md00494g. eCollection 2020 Feb 1.
A novel series of sanguinarine (SA) derivatives were synthesized and evaluated as anti-non-small cell lung cancer (NSCLC) agents. The compounds inhibited A549 and H1975 NSCLC cells with IC values of 0.96 - >30 μM and 0.79 - >30 μM, respectively. Compounds exhibited low micromolar inhibitory activity and indicated that the C6-position of SA was tolerated to be substituted by hydrophilic groups and CN. Further investigation of their mechanism of action showed that compound induced apoptosis of A549 and H1975 cells by inhibiting the Akt signaling pathway and elevating the reactive oxygen species (ROS). This study provided a strategy for developing new anti-cancer agents.
合成了一系列新型血根碱（SA）衍生物，并将其作为抗非小细胞肺癌（NSCLC）药物进行了评估。这些化合物对A549和H1975非小细胞肺癌细胞具有抑制作用，IC值分别为0.96->30 μM和0.79->30 μM。化合物表现出低微摩尔抑制活性，表明SA的C6位可被亲水基团和CN取代。对其作用机制的进一步研究表明，化合物通过抑制Akt信号通路和提高活性氧（ROS）诱导A549和H1975细胞凋亡。本研究为开发新型抗癌药物提供了一种策略。
